对人多发性骨髓瘤细胞系具有抗增殖作用的可点击细胞渗透性伪肽Pin1抑制剂的设计与合成。

IF 4.2 2区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Chemical Communications Pub Date : 2025-03-14 DOI:10.1039/d4cc05968a

Lorenzo Meneghelli , Stephanie Davidson , Anthony Gineste , Lamia El Guermah , Sabrina Kellouche-Gaillard , Franck Carreiras , Ludovic Carlier , Simon Nadal , Maud Larregola , Julien Pytkowicz , Chiara Zanato

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引用次数: 0

摘要

本文报道了一个在药物开发和生化研究中具有潜在应用价值的最小骨架、细胞可渗透、可点击的伪肽Pin1配体库的合成。用核磁共振法测定了配体的亲和常数。先导化合物4b对多发性骨髓瘤细胞系具有有效的细胞渗透性、抑制活性和抗增殖作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Design and synthesis of a clickable cell-permeable pseudopeptide Pin1 inhibitor with antiproliferative effects on human multiple myeloma cell line†

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Design and synthesis of a clickable cell-permeable pseudopeptide Pin1 inhibitor with antiproliferative effects on human multiple myeloma cell line†

The synthesis of a library of minimal-backbone, cell-permeable, clickable pseudopeptide Pin1 ligands with potential applications in drug development and biochemical studies is reported. The ligands’ affinity constants were evaluated using NMR. The lead compound , demonstrated effective cell permeability, inhibitory activity, and an antiproliferative effect on a multiple myeloma cell line.

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来源期刊

Chemical Communications 化学-化学综合

CiteScore

8.60

自引率

4.10%

发文量

2705

审稿时长

1.4 months

期刊介绍： ChemComm (Chemical Communications) is renowned as the fastest publisher of articles providing information on new avenues of research, drawn from all the world''s major areas of chemical research.